Ambeed 大中华区 CN | ZH

中文 - ZH English - EN

Ambeed.cn

搜索

关键字搜索批量搜索

首页 收藏 购物车0
首页 /
抑制剂/激动剂
肿瘤
/
MAPK/ERK Pathway
肿瘤生长增殖和凋亡
/ Raf / LXH254

LXH254 {[allProObj[0].p_purity_real_show]}

货号：A344788 同义名： Naporafenib

LXH254 is an ATP-competitive inhibitor of Raf with anti-proliferative activity. Phase I.

LXH254 化学结构 CAS号：1800398-38-2
LXH254 化学结构
CAS号：1800398-38-2
LXH254 3D分子结构
CAS号：1800398-38-2
LXH254 化学结构 CAS号：1800398-38-2
LXH254 3D分子结构 CAS号：1800398-38-2
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} 		{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

LXH254 纯度/质量文件 产品仅供科研

货号：A344788 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

• Cell Host Microbe, 2024. Ambeed. [ A163338 ]
• Cancer Res., 2024. Ambeed. [ A295334 ]
• J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]
• J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]
• JBC, 2024, 107935. Ambeed. [ A194396 ]
更多 >
产品名称 A-raf ↓ B-Raf ↓ C-Raf/Raf-1 ↓ Raf ↓ 其他靶点 纯度
Encorafenib ✔ 99%+
GDC-0879 ++++

B-Raf, IC50: 0.13 nM

 		99%+
SB-590885 ++++

B-Raf, Ki: 0.16 nM

 		99%+
RAF265 99%+
Dabrafenib ++++

B-Raf, IC50: 5.2 nM

B-Raf (V600E), IC50: 0.7 nM

 		+++

C-Raf, IC50: 6.3 nM

 		98%
Lifirafenib ++++

WT A-RAF, IC50: 1 nM

 		++

BRAF WT, IC50: 32 nM

BRAF(V600E), IC50: 23 nM

 		+++

C-RAF (Y340/341D), IC50: 7 nM

 		EGFR 98%
ZM 336372 +

C-Raf, IC50: 70 nM

 		99%+
NVP-BHG 712 +

C-Raf, IC50: 0.395 μM

 		99%+
CCT196969 +

BRAF, IC50: 0.1 μM

 		++

CRAF, IC50: 0.01 μM

 		Src 98%
Vemurafenib ++

B-Raf, IC50: 100 nM

B-Raf (V600E), IC50: 31 nM

 		+

C-Raf, IC50: 48 nM

 		98+%
PLX4720 ++

B-Raf, IC50: 160 nM

B-Raf (V600E), IC50: 13 nM

 		+++

C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM

 		BRK 99+%
GW 5074 +++

C-Raf, IC50: 9 nM

 		99%+
Avutometinib +++

BRAF, IC50: 19 nM

BRAF V600E, IC50: 8.2 nM

 		+

CRAF, IC50: 56 nM

 		98%
LY3009120 ++++

BRAF WT, IC50: 15 nM

BRAF(V600E), IC50: 5.8 nM

 		++++

C-Raf, IC50: 4.3 nM

 		99%+
Agerafenib ++

B-Raf, Kd: 36 nM

B-Raf (V600E), Kd: 14 nM

 		+

C-Raf, Kd: 39 nM

 		RET 99%+
TAK-632 +++

B-Raf, IC50: 8.3 nM

 		++++

C-Raf, IC50: 1.4 nM

 		99%+
AZ 628 +

B-Raf, IC50: 105 nM

B-Raf (V600E), IC50: 34 nM

 		++

C-Raf-1, IC50: 29 nM

 		99%
PLX7904 ✔ 98+%
Sorafenib ++

B-Raf (V599E), IC50: 38 nM

B-Raf, IC50: 22 nM

 		++++

Raf-1, IC50: 6 nM

 		++++

Raf-1, IC50: 6 nM

 		99%
Tovorafenib ✔ 99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

LXH254 生物活性

描述 RAF kinases, consisting of ARAF, BRAF, and CRAF, are key mediators in MAPK signaling cascade. LXH254 is an orally bioavailable inhibitor of both BRAF and CRAF kinases with a high degree of selectivity against a panel of 456 human kinases and in cell-based assays. Due to the capability of inhibiting both RAF monomers and dimers with similar potencies, LXH254 not only blocks MAPK activity in xenograft models harboring BRAFV600 mutation, but also exhibits inhibitory impact on mutant N- and KRAS-driven signaling[2]. The IC50 values of LXH254 against BRAF and CRAF are 0.4 and 0.2 nM, respectively. In Calu-6 cells, LXH254 stabilized BRAF-CRAF dimers with an EC50 value of 0.16 µM and inhibited cell proliferation with an EC50 value of 0.28µM. In nude rats bearing Calu-6 human NSCLC xenograft tumors, a single oral dose of LXH254 at 15, 35, 75, and 150 mg/kg reduced pMEK levels in tumors at a dose-dependent manner. Also in Calu-6 xenografts, daily treatment with LXH254 for 18 days showed dose-dependent anti-tumor activity. LXH254 at 15 and 35mg/kg resulted in 29% and 9% T/C, respectively. Administration with 75 mg/kg and 150 mg/kg LXH254 achieved mean tumor regression of 21% and 56%, respectively, compared to vehicle-treated group[1].

LXH254 动物研究

Dose Rat: 15 mg/kg - 150 mg/kg[1] (p.o.)
Administration p.o.
Pharmacokinetics
Animal Mice[1] Rats[1] Dogs[1]
Dose 2 mg/kg (i.v.)
4 mg/kg (p.o.) 		2 mg/kg (i.v.)
4 mg/kg (p.o.) 		0.2 mg/kg (i.v.)
0.4 mg/kg (p.o.)
Administration i.v.
p.o. 		i.v.
p.o. 		i.v.
p.o.
F 65% (p.o.) 38% (p.o.) 79% (p.o.)
AUCinf 4.3 μM·h (p.o.) 1.8 μM·h (p.o.) 3.1 μM·h (p.o.)
CL 19 ml/min/kg (i.v.) 31 ml/min/kg (i.v.) 3.5 ml/min/kg (i.v.)
Cmax 1.6 μM (p.o.) 0.5 μM (p.o.) 0.4 μM (p.o.)
Vss 2.1 L/kg (i.v.) 5.4 L/kg (i.v.) 1.7 L/kg (i.v.)

LXH254 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT03333343 EGFR-mutant Non-small Cell Lun... 展开 >>g Cancer 收起 << Phase 1 Recruiting May 21, 2021 Canada, Ontario ... 展开 >> Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M5G 2M9 Germany Novartis Investigative Site Recruiting Koeln, Germany, 50937 Italy Novartis Investigative Site Recruiting Ancona, AN, Italy, 60126 Novartis Investigative Site Recruiting Milano, MI, Italy, 20162 Singapore Novartis Investigative Site Recruiting Singapore, Singapore, 169610 Taiwan Novartis Investigative Site Recruiting Tainan, Taiwan, 70421 Novartis Investigative Site Recruiting Taipei, Taiwan, 10002 收起 <<
NCT02974725 Non-Small Cell Lung Cancer ... 展开 >> Melanoma 收起 << Phase 1 Recruiting June 29, 2020 United States, Massachusetts ... 展开 >> Novartis Investigative Site Recruiting Boston, Massachusetts, United States, 02114 Contact: Bakhan Barzangy    617-726-1849    bbarzangy@mgh.harvard.edu    Principal Investigator: Rebecca Heist          Australia, Victoria Novartis Investigative Site Recruiting Melbourne, Victoria, Australia, 3000 Belgium Novartis Investigative Site Recruiting Leuven, Belgium, 3000 France Novartis Investigative Site Recruiting Villejuif Cedex, France, 94805 Germany Novartis Investigative Site Recruiting Frankfurt, Germany, 60590 Novartis Investigative Site Recruiting Koeln, Germany, 50937 Italy Novartis Investigative Site Recruiting Rozzano, MI, Italy, 20089 Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08036 收起 <<
NCT02607813 NSCLC Ovarian... 展开 >> Cancer Melanoma Other Solid Tumors 收起 << Phase 1 Recruiting December 16, 2019 United States, Massachusetts ... 展开 >> Novartis Investigative Site Recruiting Boston, Massachusetts, United States, 02114 United States, New York Novartis Investigative Site Recruiting New York, New York, United States, 10021 Contact: Alida Beck       becka@mskcc.org    Principal Investigator: Gopakumar Iyer          United States, Texas UT M.D Anderson Cancer Center SC - LXH254X2101 Recruiting Houston, Texas, United States, 77030 Contact: Zehra Maloo    713-563-4426    zmaloo@mdanderson.org    Principal Investigator: Filip Janku          Canada, Ontario Novartis Investigative Site Recruiting Toronto, Ontario, Canada, M6G 1Z5 France Novartis Investigative Site Recruiting Paris, France, 75010 Novartis Investigative Site Recruiting Toulouse Cedex 9, France, 31059 Germany Novartis Investigative Site Recruiting Essen, Germany, 45147 Novartis Investigative Site Recruiting Heidelberg, Germany, 69120 Japan Novartis Investigative Site Recruiting Chuo-ku, Tokyo, Japan, 104-0045 Korea, Republic of Novartis Investigative Site Recruiting Seoul, Korea, Korea, Republic of, 03080 Netherlands Novartis Investigative Site Recruiting Groningen, Netherlands, 9713 GZ Contact: Department of Pulmonary Diseases University Medical Center Groningen    +31 503611546    h.j.m.groen@umcg.nl    Principal Investigator: H.J.M. Groen, M.D.          Medical Oncology, Erasmus MC Recruiting Rotterdam, Netherlands, 3075 CE Contact       m.dejonge@erasmusmc.nl    Principal Investigator: M. de Jonge, M.D.          Spain Novartis Investigative Site Recruiting Barcelona, Catalunya, Spain, 08035 Novartis Investigative Site Recruiting Madrid, Spain, 28007 Switzerland Novartis Investigative Site Recruiting Zuerich, Switzerland, 8091 收起 <<

LXH254 参考文献

[2]Abstract DDT01-04: Pharmacological profile and anti-tumor properties of LXH254, a highly selective RAF kinase inhibitor

LXH254 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.95mL

1.99mL

1.00mL

19.90mL

3.98mL

1.99mL

LXH254 技术信息

CAS号1800398-38-2
分子式C25H25F3N4O4
分子量 502.486
别名 Naporafenib
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 105 mg/mL(208.96 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Naporafenib | 1800398-38-2 | LXH254 | LXH 254 | LXH-254 | B/CRAF Inhibitor | MAPK/ERK Pathway | Protein Tyrosine Kinase/RTK | Raf | p38 MAPK | Bcr-Abl | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | LXH254 纯度/质量文件 | LXH254 亚型比较 | LXH254 生物活性 | LXH254 动物研究 | LXH254 临床数据 | LXH254 参考文献 | LXH254 实验方案 | LXH254 技术信息

Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
    • 客户支持
    技术支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    积分商城
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质用途提供服务。

    尊敬的 Ambeed 客户您好，
    请您选择所在区域，我们将转接对应客服为您服务！

    热门区域

    A

    B

    C

    F

    G

    H

    J

    L

    N

    Q

    S

    T

    X

    Y

    Z

    热 A B C F G H J L N Q S T X Y Z